西尼地平缓释片的处方优化及释药机制研究

发布时间：2018-03-25 05:05

本文选题：西尼地平　切入点：缓释片　出处：《中国药房》2017年25期

【摘要】：目的:优化西尼地平缓释片处方,研究其释药机制。方法:采用溶剂法制备西尼地平固体分散体,再以羟丙甲纤维素K4M(HPMC K4M)为缓释材料制备西尼地平缓释片。利用单因素法和Box-Behnken响应面法,以2、6、12 h累积释放度的综合评分为指标,筛选西尼地平缓释片处方中HPMC K4M用量、乙基纤维素(EC)用量、乳糖-微晶纤维素(MCC)比例,并进行验证。通过模型拟合的方式考察西尼地平缓释片的释药机制。结果:最优处方为西尼地平固体分散体25%、HPMC K4M 30%、EC 10%、乳糖-MCC(1∶1,m/m),黏合剂为5%的聚乙烯吡咯烷酮乙醇溶液,润滑剂为0.5%的硬脂酸镁。所制缓释片2、6、12 h时的累积释放度分别为(21.4±3.3)%、(62.9±2.8)%、(85.4±0.5)%(n=3),与预期值25%、60%、90%的相对误差分别为14.4%、4.8%、5.1%;释放曲线与一级释药模型拟合度最高,符合non-Fick扩散机制。结论:按优化后的处方成功制得具有缓释作用的西尼地平缓释片。
[Abstract]:Objective: to optimize the formulation of cinedipine sustained-release tablets and study the mechanism of its release. Methods: the solid dispersions of cilnidipine were prepared by solvent method. Cinedipine sustained release tablets were prepared by using hydroxypropylcellulose K4M(HPMC K4M as the sustained-release material. The dosage of HPMC K4M in the formulation of Xenodipine sustained-release tablets was screened by single factor method and Box-Behnken response surface method. The ratio of lactose to microcrystalline cellulose (MCCs), the amount of ethyl cellulose (EC), The drug release mechanism of the sustained-release tablets was investigated by model fitting. Results: the optimal formulation was 25 HPMC K4M30 and EC 10, lactose-MCC1: 1: 1 m / m ~ (-1), and the adhesive was 5% polyvinylpyrrolidone ethanol solution. The cumulative release rate of the sustained-release tablets was 21.4 卤3.3% at 12 h, respectively. The cumulative release rate of the sustained-release tablets was 62.9 卤2.8% and 85.4 卤0.5%, respectively, and the relative error from the expected value of 254,60,90% was 14.44.85.1.The release curve fitted best with the first-order release model. Conclusion: cilnidipine sustained-release tablets with sustained release were successfully prepared according to the optimized formulation.
【作者单位】：山东大学第二医院门诊药房;
【分类号】：R943

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